A subject of the present invention is a process for the preparation of echinocandin derivatives, the intermediates and the products obtained and their use as an antifungal medicament.
Numerous compounds having an antifungal activity are known in the prior art. In particular the echinocandin derivatives as defined in International Application WO99/29716 can be mentioned.
The objective of the present invention is to provide a new process for the preparation of echinocandin derivatives and to obtain new salts of the latter.
Echinocandin can be presented in the form of two epimers called isomer A and isomer B corresponding to the R and S configurations of the substituent in position 4. One of the subjects of the present invention is to obtain during the process, a majority of one of the two isomers, i.e. at least greater than 50% (isomer called form A, corresponding to the pharmacologically active compound of formula (I), which is not the case for the process according to WO99/29716 during which the active isomer A obtained during the process before purification on a chromatographic column is in the minority.
Moreover another objective of the present invention is to avoid purifications of the intermediate products by chromatography and to obtain crystallized products which allows a significant improvement in yields.